 |
 |
 |
 |
 |
 |
 |
|
|
|
|
|
01/03/2012
Vinco's Smart PS™ - The Smart Choice Vinco's Smart PS™ finished dosage softgels feature an exclusive fluid dispersion phosphatidylserine material that has significantly enhanced stability for maximum brain benefits. Research in animals and humans has shown.....
 Full Story
|
|
|
01/02/2012
Happy New Year! We, here at Vinco, would like to start off the New Year on the right foot by thanking you for your continued support.
Full Story
|
|
|
|
 |
|
|
|
Please enter your full email address above.
Our newsletters feature the latest news and product updates for all Vinco products.
Sign up today!
! |
|
|
|
 |
 |
 |
 |
|
|
|
Relieviate®
|
|
Item# VP-REL
60 Softgels per bottle
Dietary Supplement
Chronic Joint Pain: An American Affliction
In 2002, when the Centers for Disease Control assessed the number of chronic joint pain sufferers in the United States, the agency was surprised by its own results. Previously, the CDC had estimated that 46 million American adults, or one in five, were affected by arthritis and chronic joint symptoms. But the CDC’s state-by-state survey showed that in fact, this debilitating condition affects as many as 70 million U.S. adults, or an astonishing one in three. 1
The COX Problem
Understandably, when joint pain hit, many consumers reached for NSAIDs (non-steroidal anti-inflammatory drugs) such as aspirin, ibuprofen, and naproxen, potent inhibitors of the Cyclooxygenase or COX enzymes, which cause pain and inflammation. Unfortunately, NSAIDs aren’t selective; they inhibit both the COX-1 and COX-2 enzymes with varying intensity. So, while pain may be reduced by blocking the COX-2 enzyme, non-selective inhibition of COX-1, whose job is to protect the gastro-intestinal (GI) tract lining, can lead to dangerous side effects. As a result, GI-related adverse events are common, resulting in an estimated 103,000 hospitalizations and 16,500 deaths per year in the U.S. 2
The pharmaceutical industry’s answer to the COX problem was to develop selective COX-2 inhibitors, drugs that would shut down COX-2 enzymes but not COX-1. Prescription medications like Vioxx, Bextra and Celebrex soon became available. Unfortunately, these drugs had even worse side effects than traditional NSAIDs, dramatically increasing the risk of heart attack and stroke.
The problem was that they were too selective. By completely shutting down COX-2, these drugs are theorized to suppress production of the blood-clotting hormone prostacyclin and other cardio-protective enzymes, thus increasing cardiovascular events.
Consumers Turn To Supplements
With the prevalence of chronic joint pain and the dangers presented by pharmaceutical drugs, it’s no surprise that sales of joint health supplements have recently soared. In fact, the joint health category has surpassed calcium to become the largest market of condition-specific dietary supplements, according to a recent Packaged Facts report.3 The category was worth $174 million in 2007, up 11% from 2006 figures.
Glucosamine: Only Part Of The Puzzle
Leading the joint supplement pack is glucosamine. As a component of cartilage, glucosamine may be able to repair joint damage and prevent the progression of arthritis. However, glucosamine is not anti-inflammatory. It does not work immediately to stop the production of inflammatory prostaglandins and alleviate pain. In fact, it usually takes a minimum of eight weeks of glucosamine supplementation to feel an effect.
The Quest To Find a Plant-Derived Anti-Inflammatory Agent
Relieviate® is a proprietary supercritical hops extract that is standardized to contain a specific amount of alpha acids, the active anti-inflammatory constituents, and designed to be virtually free of phytoestrogenic and sleep-inducing compounds.
It was not developed by chance.
During the late 1990s, a handful of research companies began looking for natural ways to ease the pain of arthritis and other forms of chronic joint pain. Hundreds of different botanicals were examined. Piles of scientific literature were reviewed. And at the end of this painstaking process, about 20 candidates were identified for further study.
All of the prospects, including highly regarded botanical agents such as curcumin and boswellia, were subjected to in vitro testing to determine their anti-inflammatory potential. 4 Of those, one ingredient was identified as having the highest chance of success: a hops extract standardized to contain high amounts of naturally occurring alpha acids, Relieviate®. - Lidbury, et al.
Whole Blood Assay Reveals Suprising Result
The next step in evaluating Relieviate® efficacy was to conduct a William Harvey Modified Whole Blood Assay considered the “gold standard” for evaluating a substance’s COX activity and selectivity. There were three possible outcomes:
1. If Relieviate® moderately inhibited both COX-1 and COX-2, then it could be assumed to cause the same GI problems as traditional NSAIDs.
2. If Relieviate® shut down COX-2 completely without affecting COX-1, it could be assumed to cause the same cardiovascular events as selective COX-2 inhibitors like Vioxx, Bextra and Celebrex.
3. However, if Relieviate® could moderately inhibit COX-2 while only mildly inhibiting COX-1, then the researchers would have a winner.
The results? Relieviate® achieved the perfect middle ground. It inhibited COX-2 strongly enough to be able to alleviate pain, but not so strongly that it shut down the enzyme altogether. And it only mildly inhibited COX-1, so GI toxicity was extremely unlikely.5 Having passed these initial hurdles, Relieviate® was ready for the final test: human clinical trials.
Relieviate® Human Clinical Research
Study #1: A dietary supplement is a selective COX-2 inhibitor both in vitro and ex vivo in healthy human volunteers.
A second double-blind, randomized parallel design trial was conducted on 19 healthy subjects. 6 This time, subjects received a single dose of ibuprofen (400 mg), a soft gel containing hops resin (450 mg) or a capsule containing the hops resin converted to powder form (300 mg 4x/day). Both supplement forms were
standardized for hops alpha acids (150 mg). Once again, levels of COX-1 and COX-2 were monitored at regular intervals over nine hours after the initial dose.
Results
The hops preparations were as effective as ibuprofen at inhibiting COX-2, but had significant COX-1 sparing activity over a nine-hour period. It was interesting to note that the hops resin soft gel was only administered once, whereas the hops powder capsules were administered in four divided doses over a nine-hour time period. The soft gel had a faster onset of action and gradually reduced pain-causing enzymes over the period of the study. This improved activity of the soft gel was probably the result of the natural state of the resin, solubilized in oil, as opposed to the conversion of resin-to-powder for capsules and tablets.
Relieviate® Human Clinical Research
Study #2: Efficacy of oral Relieviate® intake in subjects with knee osteoarthritis: a randomized, double-blind study
After successful in vitro and ex vivo trials, it was time to put Relieviate® to the ultimate test: Would it alleviate pain in subjects with arthritis?
A double-blind, placebo-controlled randomized trial evaluated the pain-relieving effects of 14 days of Relieviate® oral supplementation. 7 Thirty-six subjects with osteoarthritis of the knee participated in the study. At baseline, they completed a Western Ontario McMasters Osteoarthritis Index (WOMAC) questionnaire to evaluate pain levels. The time to perform a 20-meter walk on a flat surface was also recorded.
Study participants were assigned to take Relieviate® or a placebo. They were told to discontinue taking NSAIDs during the study period; however, up to 2,000 mg of acetaminophen could be taken for pain relief, limited to two days per week (rescue medication).
On day 15, the time to perform a 20-meter walk on a flat surface was again measured and improvements in pain relief were assessed using the WOMAC
questionnaire.
Results
• Relieviate® intake showed a fast-acting effect on mean pain relief; significant improvement over placebo could be measured only two hours after the first ingestion.
• 1,000 mg per day of Relieviate® significantly improved parameters of osteoarthritis pain, including mean pain relief while in bed, sitting, lying, and
walking on a flat surface.
• The effectiveness of Relieviate® was supported by the limited use of rescue medication in the treatment groups compared to placebo.
• The researchers concluded that Relieviate® improved pain relief in patients with osteoarthritis, with the ultimate outcome of increased function and better
quality of life.
Mechanism Of Action
Pain is caused by the activation of COX enzymes. Without primarily inhibiting the COX-2 pathway, there can be no fast pain reduction. In vitro and ex vivo studies reveal that Relieviate®:
• Moderately inhibits COX-2, thus reducing pain-causing enzymes without creating cardiovascular risk
• Mildly inhibits COX-1, thus dramatically reducing the likelihood of GI adverse effects
Bioavailability
In vitro testing, utilizing the CACO-2 cell monolayer assay, indicates that the permeability of the alpha acids contained in Relieviate® is high. High permeability predicts good human oral bioavailability.
Safety
Relieviate® safety has been confirmed in a double-blind placebo-controlled human clinical trial. The comparison of pre- and post-supplementation blood work, as well as adverse side effect monitoring, showed that Relieviate® was well-tolerated and led to no GI discomfort.
Additionally, studies in rats and dogs have demonstrated that hops alpha acids caused no changes in hematological examinations, blood chemistry, urine tests, or pathological examinations, and are non-toxic even in doses that far
exceed the amount found in Relieviate®. Hops alpha acids have also tested negative for mutagenicity (the ability to cause mutations) and genotoxicity (the ability to cause genetic damage).
Purity
Relieviate® is made from hops that are grown in the United States, inspected by the USDA, and fully traceable to the farm where they are cultivated. The hops are extracted in an ISO-certified facility, using a super critical extraction process that is free of chemical solvents. The finished product is subjected to heavy metal analysis and regularly screened for the presence of 73 different pesticides.
Relieviate® Soft Gel Highlights
Relieviate® soft gels contain a proprietary hops resin extract standardized to alpha acids, key anti-inflammatory constituents, clinically demonstrated to have a fast acting pain-relieving effect in patients with arthritis.
Research has shown that Relieviate®
• Moderately inhibits the pain-causing enzyme COX-2, thus relieving chronic joint pain
• Only mildly inhibits the GI-protective enzyme COX-1, thus avoiding GI distress
• Significantly improves parameters of osteoarthritis pain, with the ultimate outcome of increased function and better quality of life
Directions for Use
As a dietary supplement for adults and children twelve or more years of age, take one or two softgels per day, or as directed by a qualified healthcare professional.
References
1. Arthritis and chronic joint symptoms more common than previously thought. Centers for Disease Control. Oct. 24, 2002. http://www.cdc.gov/media/pressrel/r021024.htm
2. Wolfe MM, et. al. Gastrointestinal toxicity of nonsteroidal anti-inflammatory drugs. NEJM. 1999 Jun 17;340(24):1888-99.
3. Heller, Lorraine. New report breaks down US supplement market. Nutraingredients-usa.com. Aug. 21, 2008. http://www.nutraingredients-usa.com/ Consumer-Trends/New-report-breaks-down-US-supplement-market
4. Lemay M, et al. Cyclooxygenase inhibiting activity of anti-inflammatory dietary supplements: Ex vivo evaluation. Nutrilite Health Institute, Access Business Group LLC, Buena Park CA.
5. Lidbury, et al. The effects of AH88 on the activity of COX-1 and COX-2 using human whole blood and A549 cells. Pharmachem Laboratories, Kearny NJ.
6. Lemay M, et al. A dietary supplement is a selective COX-2 inhibitor both in vitro and ex vivo in healthy human volunteers. Nutrilite Health Institute, Access Business Group LLC, Buena Park CA.
7. Jager R, Purpura M. Efficacy of Oral Perluxan Intake in Subjects With Knee Osteoarthritis: A Randomized, Double-Blind Study. Pharmachem Laboratories, Kearny, NJ.
|
|
|
|
